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summary medical pharmacology
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Summary Medical pharmacologyLecture 1: Intro to medicines
(Medical) Pharmacology
Explanation of action of Pharmaca (=biologically active substances, including toxins) in the
human (or animal) body
• Medicine = pharmacon (“drug”) applied for therapy
• Pharmacodynamics = “what does the drug do with the body”
• Pharmacokinetics = “what does the body do with the drug”
General pharmacology= pharmacodynamic + pharmacokinetics
Pharmacotherapy = Applied Pharmacology
Use of knowledge and insights gained from pharmacology for the treatment of diseased
humans (or animals) in a responsible, effective and safe manner. In other words:
pharmacology applies in practice the knowledge about the drug that was received from
pharmacology. (Outweigh benefits with adverse effects)
History of pharmacology
- Pharmaceutical industry: provides synthetic drugs (based on synthetic chemistry)
- Biopharmaceutical industry: provides synthetic drugs by applying molecular
biological techniques
- Chemistry: provide the means to investigate the active parts in the remedies.
- Biomedical sciences: biomedical information to work out the relationship between
these active products and the application of certain areas (e.g., animal models, cell
models, diseases, and symptoms).
,What is pharmacology?
- Pharmacology is the study of what drugs do and how they do it
- A drug is a chemical that is usually used to treat disease
- Drugs are intended to have a selective action but this ideal is seldom achieved
- There is always a risk of adverse effects as well as a benefit connected with using
any drug (because of dose etc.)
- Knowledge of pharmacology is essential for using drugs effectively in therapy
Pharmacology involves a lot of conceptual thinking. ;Cp: concentration of drug in the blood.
Therapeutic window: most drugs have a direct relationship between the concentration of
the drug in the blood plasm and its therapeutic effect. The drug should be above the
minimum effective concentration and under the minimum toxic concentration. The
therapeutic effects will be optimal and the benefit-risk ratio at its maximum.
Effects of Medicines/Drugs (1)
- Primary effect= effect(s) for which the compound is administered; therapeutic
reason
- Side effect = adverse/unwanted effect(s)
The distinction between primary effect and side effect is determined by the aim for which
the medicine is administered
- e.g., acetylsalicylic acid (aspirin) as a pain killer (=analgetic) or against blood
clotting (=anti-coagulant)
Effects of Medicines/Drugs (2)
- Placebo= a preparation without any pharmacologically active substance
- Nocebo = a placebo with unwanted effects (= side effects) (no active substance)
A) placebo may have a (therapeutic) effect =PLACEBO EFFECT
b) Expectations of the patient (to a large extent) determine the strength of the placebo
effect
c)The contribution of the placebo effect to the overall effects of a drug are investigated in
“randomized, placebo-controlled clinical trials” (Phase III = RCT)
,IND: Investigational New Drug Application (IND) is a request from a clinical study sponsor to
obtain authorization from the Food and Drug Administration (FDA) to administer an
investigational drug or biological product to humans.
NDA: New Drug Application (NDA)
Drugs discovery (2-5 years)
Drug development (5-9 years)
Drug development takes on average 7-14 years from the inception of the idea to FDA
approval
EDA (Europe approval)
, Lecture 2: Drugs dose effect & Receptor theory
Pharmacodynamics: what does the drug do with the body
The four levels of drug action and drug classification
Mechanism Definition Response component
System An effect on system function Integrated systems including linked systems
(e.g., nervous system, cardiovascular system)
Tissue An effect on tissue function Electrogenesis, contraction, secretion,
metabolic activity, proliferation
Cellular Transduction The biochemicals linked to the drug target
(e.g., ion channels, enzyme, G proteins)
Molecular Interaction with the drug’s The drug target (e.g., receptor, ion channel,
molecular target enzyme, carrier, molecule)
You need to know all the effects of the drug at all levels to provide a drug with the most
optimal effects. But if you want to apply this knowledge in drug development then you have
to go back to the molecular level. Drug effects belong to the category of a complex
phenomenon because all together there are at least 4 levels where you can establish the
effects of drugs. But for the purpose of thermodynamics, it is the molecular level that is
essential because at that level we can really identify what kind of drug target and compound
interferes with the drug.
Targets for drug action
An agonist alters the form of the receptor and thereby activates the receptor.
An antagonist binds to the receptor but doesn’t alter the conformation, there will be no
effect and no transduction mechanism. However, it will prevent binding of agonist mediators
Modulator: the ion channel will be open or closed after binding a modulator.
Pro-drugs are handy for localized drug use (e.g., Parkinson's disease).
False substrates: like Amphetamine (effect on dopamine); cocaine is a transport inhibitor
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